Pd(II)-catalyzed aerobic oxidative intramolecular hydroamination and C-H functionalization of N-alkynyl anilines for the synthesis of indole derivatives

A Pd(II)-catalyzed aerobic oxidative approach to 2,3-dihydro-1H-pyrrolo[1,2-a]indoles from simple N-alkynyl anilines through tandem intramolecular hydroamination and aryl C-H activation process has been developed. Molecular oxygen was used as the sole oxidant to recycle the Pd-catalysis. This protocol is attractive due to the available starting materials and the valuable products.